通过对价格昂贵的没食子儿茶素没食子酸酯(-)-GCG进行一步甲基化制备全甲基化(-)-GCG成本较高,所以本文选取对绿茶粗提物进行乙酰化和甲基化2种方法来制备全甲基化(-)-GCG,其中甲基化方法产率达到7.6%,是获得全甲基化(-)-GCG较简单经济的途径,为(-)-GCG的衍生化修饰及其MDR逆转活性的研究提供基础,所合成的化合物均经核磁共振氢谱、碳谱、质谱以及旋光对其结构进行了验证。
Preparation of permethyl (-)-gallocatechin gallate by one-step methylation from comercial (-)-gallocatechin gallate ((-)-GCG) is expensive. Two methods were deceloped to obtain permethyl (-)- GCG) from crude extract of green tea= the acetylation and the methylation. The methylation method is economical and the yield is high to 7. 6%, which provide the basis for synthesis of (-)-GCG derivatives and study of their reversal activity of multidrug resistance. The synthetic compounds were identified by 1H-NMR, 13C-NMR, mass spectrometry, and optical rotation.